Efavirenz (DMP 266) is a Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor. The mechanism of action of efavirenz is as a Non-Nucleoside Reverse Transcriptase Inhibitor, and Cytochrome P450 3A Inducer, and Cytochrome P450 2B6 Inducer, and Cytochrome P450 2C9 Inhibitor, and Cytochrome P450 2C19 Inhibitor, and Cytochrome P450 3A4 Inhibitor. The chemical classification of efavirenz is Non-Nucleoside Analog.

HIV-1:2.93 nM (Ki)

Efavirenz对培养的胶质母细胞瘤和分化的神经母细胞瘤细胞系的线粒体呼吸功能具有直接抑制作用[2]。ER应激标志物，包括CHOP和GRP78的表达（蛋白和mRNA），eIF2a的磷酸化，以及XBP1剪接形式的存在均上调。Efavirenz还增加了细胞质Ca2+含量，并诱导了ER形态学变化，这暗示了ER应激。这种反应在具有改变的线粒体功能（Rho）的细胞中大大减弱。Efavirenz对ER的影响，特别是与线粒体参与相关的影响，与标准药理学ER应激诱导剂引发的影响不同[3]。

Efavirenz导致动脉硬化，但在所测试的剂量和持续时间内，并未导致ApoE(-/-)小鼠[4]的斑块进展增加。

Recombinant RT enzymes are expressed, purified, and assessed for inhibition by Efavirenz (L-743726). Ki and Kii values are determined for each enzyme tested. The wild-type RT exhibited exclusively noncompetitive inhibition kinetics (data not shown), and, therefore, the Ki and Kii values are identical. Pure noncompetitive inhibition is not assumed for the mutant enzymes, and, hence, the values of both Ki and Kii are obtained from the linear mixed-type inhibition equation. The two- to threefold differences between the Ki and Kii values probably reflect a small contribution of competitive inhibition with the mutant RTs[1].

The OCR(O2 consumption rate) is measured in SH-SY5Y and U-251 mg cells exposed to vehicle, 10 μM efavirenz or 25 μM efavirenz for 1 h. (Only for Reference)